| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
TLR4/NF‑kappaB pathway, Nrf2/ARE pathway, and ROS scavenging. Bixin does not bind to a single receptor but modulates multiple signaling cascades involved in inflammation and oxidative stress.
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| ln Vitro |
In vitro, bixin induces apoptosis in several cancer cell lines, including A549 (lung), HeLa (cervical), and MCF‑7 (breast) cells. It suppresses LPS‑induced production of pro‑inflammatory cytokines (TNF‑alpha, IL‑6, IL‑1beta) in macrophages by inhibiting NF‑kappaB activation. Bixin also upregulates Nrf2 and its downstream antioxidant enzymes (HO‑1, NQO1), thereby reducing intracellular ROS levels. At concentrations of 1-50 microM, it shows dose‑dependent cytoprotective and anti‑inflammatory effects without significant cytotoxicity in normal cells.
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| ln Vivo |
In vivo, bixin has been shown to improve cardiac function and reduce myocardial injury in mice fed a high‑fat diet. Oral administration of bixin (10-50 mg/kg/day) for 8-12 weeks attenuated cardiac hypertrophy, fibrosis, and oxidative stress. It also lowered serum lipid levels, decreased inflammatory markers, and enhanced antioxidant enzyme activities. In tumor xenograft models, bixin inhibited tumor growth, although these studies are less extensive. Its insulin‑sensitizing effects have been observed in diabetic animal models.
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| Enzyme Assay |
Since bixin is a natural product with pleiotropic effects, specific enzyme/receptor binding assays are not standard. To study its mechanism, cells are treated with bixin (1-50 microM) and then stimulated with LPS (1 microg/mL) for inflammatory studies. NF‑kappaB activation is assessed by Western blot for p‑IkappaBalpha and p65 nuclear translocation. Nrf2 activation is evaluated by measuring HO‑1 and NQO1 protein levels. ROS production is quantified using the DCFH‑DA fluorescent probe. For direct antioxidant capacity, chemical assays such as DPPH and ABTS radical scavenging are performed. Binding to TLR4 can be assessed by molecular docking or surface plasmon resonance, but these are not routine.
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| Cell Assay |
Cancer cell lines (A549, HeLa, MCF‑7) or RAW 264.7 macrophages are seeded in 96‑well plates and cultured overnight. Cells are treated with bixin at concentrations of 1, 5, 10, 25, and 50 microM for 24-48 h. Cell viability is measured by MTT assay. For apoptosis, cells are stained with Annexin V‑FITC and propidium iodide and analyzed by flow cytometry. Caspase‑3/7 activity is measured using a fluorogenic substrate. In macrophage assays, cells are pre‑treated with bixin for 1-2 h, then stimulated with LPS (1 microg/mL) for 6-24 h. Culture supernatants are collected for cytokine quantification by ELISA. Cell lysates are used for Western blot analysis of signaling proteins.
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| Animal Protocol |
In vivo studies are typically performed in male C57BL/6 mice fed a high‑fat diet (60% kcal from fat) for 12-16 weeks. Bixin is suspended in 0.5% carboxymethylcellulose or corn oil and administered by oral gavage at doses of 10, 25, or 50 mg/kg once daily. Body weight and food intake are recorded weekly. At the end of the study, blood is collected for serum biochemical analysis (glucose, insulin, lipid profile, inflammatory cytokines). Hearts are excised for histology (H&E, Masson's trichrome for fibrosis) and molecular analysis (qPCR for inflammatory and antioxidant genes, Western blot for protein expression). Echocardiography may be performed to assess cardiac function. For tumor studies, xenograft models are used with similar dosing regimens.
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| ADME/Pharmacokinetics |
Bixin has molecular formula C2₅H30O4 and molecular weight 394.50. It is a lipophilic compound with poor aqueous solubility; it is soluble in organic solvents like DMSO, ethanol, and oils. Oral bioavailability is low due to extensive first‑pass metabolism and poor absorption, but it can be detected in plasma after high doses. The compound is light‑sensitive and should be stored protected from light. Its half‑life in vivo is short, and it is rapidly metabolized to norbixin and other derivatives.
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| Toxicity/Toxicokinetics |
Bixin is generally recognized as safe (GRAS) as a food additive. In pharmacological studies, no significant acute toxicity has been observed at doses up to 500 mg/kg in rodents. Chronic administration at high doses may cause mild gastrointestinal disturbances. It is not genotoxic or carcinogenic in standard assays. However, as a research compound, it is not intended for human therapeutic use; proper laboratory safety measures should be taken.
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| References | |
| Additional Infomation |
Bixin is a carotenoid acid, specifically the 6'-monomethyl ester of 9'-cis-6,6'-dicoranin-6,6'-diacid. It possesses antioxidant, insulin-sensitizing, biopigment, anti-inflammatory, edible pigment, and apoptosis-inducing effects. It is a carotenoid acid, a dicarboxylic acid monoester, and a methyl ester. Bixin is found in the annatto tree (Bixa orellana) and the Chinese honeybee (Apis cerana), and relevant data have been reported. See also: annatto seeds (partial).
Bixin is a natural carotenoid from annatto seeds with a wide range of biological activities, including anti‑inflammatory, antioxidant, anti‑cancer, and insulin‑sensitizing effects. It is widely used as a food colorant and has attracted scientific interest for its potential cardiovascular and metabolic benefits. Mechanistically, it modulates TLR4/NF‑kappaB and Nrf2 pathways and reduces oxidative stress. Bixin is available as a research‑grade natural product for in vitro and in vivo studies, but it is not an approved drug. Its stability and solubility issues are key considerations in experimental design. |
| Molecular Formula |
C25H30O4
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|---|---|
| Molecular Weight |
394.5033
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| Exact Mass |
394.214
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| CAS # |
6983-79-5
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| PubChem CID |
5281226
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| Appearance |
Brown to reddish brown solid powder
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| Density |
1.035 g/cm3
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| Boiling Point |
596ºC at 760 mmHg
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| Melting Point |
217ºC (dec.)
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| Flash Point |
197.8ºC
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| Index of Refraction |
1.548
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| LogP |
5.81
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
29
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| Complexity |
823
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C/C(=C\C=C\C=C(/C)\C=C\C=C(\C)/C=C/C(=O)OC)/C=C/C=C(\C)/C=C/C(=O)O
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| InChi Key |
RAFGELQLHMBRHD-SLEZCNMESA-N
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| InChi Code |
InChI=1S/C25H30O4/c1-20(12-8-14-22(3)16-18-24(26)27)10-6-7-11-21(2)13-9-15-23(4)17-19-25(28)29-5/h6-19H,1-5H3,(H,26,27)/b7-6+,12-8+,13-9+,18-16+,19-17+,20-10+,21-11+,22-14+,23-15-
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| Chemical Name |
(2E,4E,6E,8E,10E,12E,14E,16Z,18E)-20-methoxy-4,8,13,17-tetramethyl-20-oxoicosa-2,4,6,8,10,12,14,16,18-nonaenoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~7.14 mg/mL (~18.10 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 0.71 mg/mL (1.80 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.1 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 0.71 mg/mL (1.80 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.1 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5349 mL | 12.6743 mL | 25.3485 mL | |
| 5 mM | 0.5070 mL | 2.5349 mL | 5.0697 mL | |
| 10 mM | 0.2535 mL | 1.2674 mL | 2.5349 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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